| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
L-Asparaginase targets L-asparagine, an amino acid that is essential for the growth and survival of certain cancer cells, such as acute lymphoblastic leukemia cells. These cells lack the enzyme asparagine synthetase and cannot synthesize their own asparagine. By depleting L-asparagine from the plasma, L-asparaginase starves the cancer cells, leading to inhibition of RNA and DNA synthesis and subsequent apoptosis.
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| ln Vitro |
AML blast cells and LSC subsets are cytotoxically affected by L-asparaginase [1]. This impact is mediated by L-asparaginase on MSC, monocyte/macrophage fractions, and CD34+CD38+ and CD34+CD38+ LSC fractions [1]. 】.
In vitro, L-Asparaginase is characterized by its enzymatic activity. It catalyzes the hydrolysis of L-asparagine to L-aspartic acid and ammonia. Its activity is measured by the amount of ammonia produced or by the decrease in asparagine concentration. It is used in cell culture to study the effects of asparagine depletion on cell growth and metabolism. |
| ln Vivo |
In vivo, L-Asparaginase is used as a therapeutic agent for the treatment of acute lymphoblastic leukemia (ALL). It is administered intravenously or intramuscularly. By depleting plasma asparagine, it inhibits protein synthesis in leukemic cells, leading to cell death. It is a key component of combination chemotherapy regimens for ALL.
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| Enzyme Assay |
The in vitro enzyme activity assay for L-Asparaginase involves incubating the enzyme with L-asparagine as a substrate. The reaction is carried out in a suitable buffer at an optimal pH and temperature. The amount of ammonia produced is measured using a colorimetric method, such as the Nessler's reagent or the Berthelot reaction. One unit of activity is defined as the amount of enzyme that produces 1 μmol of ammonia per minute under the assay conditions.
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| Cell Assay |
In vitro cell culture studies for L-Asparaginase are performed in leukemia cell lines that are dependent on exogenous asparagine. Cells are treated with the enzyme, and cell viability is assessed using an MTT or trypan blue exclusion assay. The depletion of asparagine from the culture medium is confirmed by HPLC. The effect on protein synthesis and apoptosis is assessed by Western blotting and flow cytometry.
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| Animal Protocol |
In vivo animal experiments for L-Asparaginase are performed in mouse models of leukemia. The enzyme is administered intravenously or intraperitoneally, and its effect on tumor growth and survival is assessed. The depletion of plasma asparagine is measured. The efficacy of L-asparaginase in combination with other chemotherapeutic agents is also evaluated.
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| ADME/Pharmacokinetics |
L-Asparaginase is an enzyme with a molecular weight that varies depending on the source. It is typically supplied as a lyophilized powder or in aqueous solution. It is soluble in water and aqueous buffers. It is typically stored at 2-8°C for short-term stability and at -20°C for long-term stability. Its activity is optimal at pH 7.0-8.0.
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| Toxicity/Toxicokinetics |
Toxicological data for L-Asparaginase indicate that it can cause significant side effects, including hypersensitivity reactions, pancreatitis, liver toxicity, and coagulation disorders. These toxicities are related to its mechanism of action and its effects on protein synthesis. It is contraindicated in patients with a history of pancreatitis or hypersensitivity to the drug.
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| References | |
| Additional Infomation |
L-Asparaginase is an approved drug for the treatment of acute lymphoblastic leukemia (ALL). It is available in various formulations, including native and pegylated forms. It is a key component of combination chemotherapy regimens for ALL. It is also used in some veterinary applications. Its role in depleting asparagine makes it a unique and important anticancer agent.
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| Exact Mass |
151.009
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|---|---|
| CAS # |
9015-68-3
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
204.5±23.0 °C at 760 mmHg
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| Flash Point |
77.5±22.6 °C
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| Vapour Pressure |
0.2±0.4 mmHg at 25°C
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| Index of Refraction |
1.745
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| LogP |
1.78
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| InChi Key |
QXLQZLBNPTZMRK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H19NO/c1-10-6-7-13(11(2)8-10)14(16)12(3)9-15(4)5/h6-8H,3,9H2,1-2,4-5H3
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| Chemical Name |
2-[(dimethylamino)methyl]-1-(2,4-dimethylphenyl)prop-2-en-1-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
0.1 M HCL : 50 mg/mL
H2O : ~1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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